(19)
(11) EP 0 770 602 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
14.05.1997 Bulletin 1997/20

(43) Date of publication A2:
02.05.1997 Bulletin 1997/18

(21) Application number: 96307583.3

(22) Date of filing: 18.10.1996
(51) International Patent Classification (IPC)6C07D 211/70
(84) Designated Contracting States:
AT BE CH DE DK ES FR GB GR IE IT LI NL PT SE

(30) Priority: 23.10.1995 JP 274175/95
03.10.1996 JP 263010/96

(71) Applicant: Ajinomoto Co., Inc.
Tokyo 104 (JP)

(72) Inventors:
  • Fujii, Akiko, c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Kubo, Mie, c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Yamamoto, Tomoya c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Shimada, Jiro c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Mihara, Ryuichi c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Naora, Hirokazu c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)
  • Asai, Koji c/o Central Research Laboratories
    Kawasaki-ku,Kawasaki-shi, Kanagawa-ken (JP)

(74) Representative: Nicholls, Kathryn Margaret et al
MEWBURN ELLIS York House 23 Kingsway
London WC2B 6HP
London WC2B 6HP (GB)

   


(54) Crystals of piperidine derivatives, intermediates for production of the same, and process for producing the same


(57) The invention provides monohydrate and trihydrate crystals of N-(2-(4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)piperidino)ethyl)-1-formyl-4-piperidinecarboxamide hydrochloride. It also provides crystalline anhydride intermediates for the production of the mono- and trihydrates.
The monohydrate and trihydrate crystals of the present invention exhibit excellent stability. The monohydrate exhibits excellent oral absorption, and the trihydrate exhibits a high dissolution rate, making them suitable for use in drug products to meet various requirements.





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